Table 2. Kinase Selectivity of the Preferred Compounds.
|
Kinase IC50a (nM)(Selectivity (fold vs JAK2)) |
|||||
|---|---|---|---|---|---|
| Compd | JAK1 | JAK2 | JAK3 | TYK2 | FLT3 |
| A2 | 43 (6.1) | 7 | 54 (7.7) | 43 (6.1) | 108 (15.4) |
| A4 | 73 (24.3) | 3 | 166 (55.3) | 33 (10) | 206 (68.7) |
| A6 | 106 (21.6) | 8 | 208 (41.6) | 77 (9.6) | 320 (40) |
| A7 | 87 (21.7) | 4 | 156 (39) | 62 (15.5) | 311 (77.7) |
| A8 | 193 (38.6) | 5 | 273 (54.6) | 206 (41.2) | 467 (93.4) |
| A9 | 142 (23.7) | 6 | 287 (47.8) | 192 (32) | 412 (68.7) |
| A12 | 178 (35.6) | 5 | 265 (53) | 204 (40.8) | 297 (59.4) |
| 13ac | 42 (14) | 3 | 94 (31) | 75 (25) | 62 (20.7) |
a
IC50 data are detected by Eurofins Discovery.